bazedoxifene/conjugated estrogens

Duavee

Classification

Indications

Treatment of moderate/severe vasomotor symptoms of menopause in female patients with an intact uterus. Prevention of postmenopausal osteoporosis in female patients with an intact uterus (supplemental calcium and vitamin D recommended if dietary intake is not adequate).

Action

Both bazedoxifene and conjugated estrogens bind to α and β estrogen receptors. Conjugated estrogen acts as an agonist at these receptors. Bazedoxifene acts as an agonist in some tissues and an antagonist in other tissues, including the uterus. The combined effect is estrogen replacement while minimizing the risk of endometrial hyperplasia and prevention of postmenopausal osteoporosis.

Therapeutic effects

Reduced vasomotor symptoms of menopause with reduced risk of endometrial hyperplasia and prevention of postmenopausal osteoporosis.

Time/action profile (effect on vasomotor symptoms†)

ROUTE

ONSET

PEAK

DURATION

PO

within 4 wk

12 wk

duration of treatment

†effects on osteoporosis were noted at 12–24 mos and lasted throughout treatment (5 yr)

Contraindications/Precautions

Contraindicated in: Undiagnosed/abnormal vaginal bleeding;Not recommended for use in hepatic or renal impairment or BMI > 27 kg/m2 (↑ risk of endometrial hyperplasia;History of known/suspected breast cancer or other estrogen-dependent cancer;Active or past history of thromboembolism including stroke, myocardial infarction or pulmonary embolism; Known protein C, protein S or antithrombin deficiency or other thrombophilic disorders; Geriatric: not recommended for use in patients ≥ 75 yr, has been associated with dementia in patients ≥ 65 yr Obstetric: May cause fetal harm, do not use during pregnancy or in women who may become pregnant. Lactation: Estrogen enters breast milk, should not be used in breastfeeding women.

Ear, Eye, Nose, Throat

Gastrointestinal

Dermatologic

hot flash (most frequent)

Fluid and Electrolyte

hypocalemia

Musculoskeletal

muscle spasms

neck pain

Interactions

Bazedoxifene

Drug-Drug interaction

Concurrent use with UGT inducers including carbamazepine, phenobarbital, phenytoin and rifampin may ↓ levels and result in ↑ risk of endometrial hyperplasia (monitoring during long term concurrent use is recommended)

Interactions

Conjugated estrogens

Drug-Drug interaction

Concurrent use with CYP3A4 inhibitors including clarithromycin, erythromycin, itraconazole, , ketoconazole or ritonavir may ↑ levels of conjugated estrogens and the risk of endometrial hyperplasia (monitoring during long term concurrent use is recommended)Concurrent use with CYP3A4 inducers including carbamazepine, phenobarbital, and rifampin may ↓ effectiveness and alter uterine bleeding patterns. Concurrent use of progestins, other estrogens or estrogen agonist/antagonists may alter the effectiveness or treatment and/or ↑ risk of adverse reactions and should be avoided.Concurrent use with St. John's wort may ↓ effectiveness and alter uterine bleeding patterns.Concurrent use with grapefruit juice may ↑ levels of conjugated estrogens and the risk of endometrial hyperplasia.

Potential Nursing Diagnoses

Implementation

Oral: Administer once daily without regard to meals. Swallow tablets whole; do not crush, break, or chew.

Patient/Family Teaching

Instruct patient to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Advise patient to keep Duavee in original container to protect from moisture; avoid placing in pill boxes or organizers. Open only one blister pouch and one tablet at a time; record date opened and discard after 60 days.

Advise patient to avoid grapefruit juice during therapy.

Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of Rx, OTC, and herbal products, especially progestins, additional estrogens, or additional estrogen agonist/antagonists without consulting health care professional; may increase risk of uterine cancer.

Caution patient that cigarette smoking during estrogen therapy may increase risk of serious side effects, especially for women over age 35.

Advise patient treated for osteoporosis that exercise has been found to arrest and reverse bone loss. Discuss any exercise limitations with health care professional before beginning program.

Emphasize the importance of routine follow-up physical exams, including BP; breast, abdomen, and pelvic examinations; Papanicolaou smears every 6–12 mo; and mammogram every 12 mo or as directed. Health care professional will evaluate possibility of discontinuing medication every 3–6 mo.

Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. May cause fetal harm.

Evaluation/Desired Outcomes

Reduction in frequency and intensity of moderate to severe hot flashes.

Decreased risk of development of osteoporosis.

Therapy should be used for the shortest time possible and need for therapy evaluated regularly.

Stuenkel talks about two of the newer SERM options--ospemifene for dyspareunia and a combination of the SERM bazedoxifene and conjugated equine estrogens that's available outside of the United States--to treat vasomotor symptoms or for prevention of bone loss.

The findings by Duke Cancer Institute indicate that the drug bazedoxifene packs a powerful one-two punch that not only prevents estrogen from fueling breast cancer cell growth, but also flags the estrogen receptor for destruction.

Use of a combination of bazedoxifene and conjugated estrogens had no significant impact on breast density (a potential risk factor for breast cancer) in postmenopausal women, based on data from the SMART-5 trial.

Some of the more promising compounds are Tygacil, a broad-spectrum antibiotic; Lybrel, a low-dose oral contraceptive; bazedoxifene for osteoporosis and menopausal symptoms; and Pristiq for depression and other neurological disorders.

All content on this website, including dictionary, thesaurus, literature, geography, and other reference data is for informational purposes only. This information should not be considered complete, up to date, and is not intended to be used in place of a visit, consultation, or advice of a legal, medical, or any other professional.